scholarly journals Carbonic Anhydrase Inhibitors. Part 551 Metal Complexes of 1,3,4-Thiadiazole-2-Sulfonamide Derivatives: In Vitro Inhibition Studies With Carbonic Anhydrase Isozymes I, II and IV

1998 ◽  
Vol 5 (2) ◽  
pp. 103-114 ◽  
Author(s):  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Fabrizio Briganti ◽  
Marc A. Ilies ◽  
Andrei Jitianu
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Coordination Compounds ◽  
Active Sites ◽  
Carbonic Anhydrase Inhibitors ◽  
Standard Procedures ◽  
In Vitro Inhibition ◽  
Characteristic Features ◽  
Inhibition Studies

Coordination compounds of 5-chloroacetamido-1,3,4-thiadiazole-2-sulfonamide (Hcaz) with V(IV), Cr(lll), Fe(ll), Co(ll), Ni(ll) and Cu(ll) have been prepared and characterized by standard procedures (spectroscopic, magnetic, EPR, thermogravimetric and conductimetric measurements). Some of these compounds showed very good in vitro inhibitory properties against three physiologically relevant carbonic anhydrase (CA)isozymes, i.e., CA I, II, and IV. The differences between these isozymes in susceptibility to inhibition by these metal complexes is discussed in relationship to the characteristic features of their active sites, and is rationalized in terms useful for developing isozyme-specific CA inhibitors.

Carbonic anhydrase inhibitors: in vitro inhibition of α isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids

2011 ◽  
Vol 28 (2) ◽  
pp. 283-288 ◽  
Author(s):  
Derya Ekinci ◽  
Lutfi Karagoz ◽  
Deniz Ekinci ◽  
Murat Senturk ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Inhibitors ◽  
In Vitro Inhibition

scholarly journals Metal Complexes of 1,3,4-Thiadiazole-2,5-Disulfonamide are Strong Dual Carbonic Anhydrase Inhibitors, although the Ligand Possesses very Weak such Properties

1995 ◽  
Vol 2 (6) ◽  
pp. 331-336 ◽  
Author(s):  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Coordination Compounds ◽  
Uv Spectroscopy ◽  
Carbonic Anhydrase Inhibitors ◽  
Strong Dual ◽  
Ir And Uv Spectroscopy ◽  
Parent Ligand

Coordination compounds of Co(II), Ni(II), Cu(II), Zn(II), and Cd(II) with 1,3,4-thiadiazole-2,5-disulfonamide as ligand were synthesized and characterized by IR and UV spectroscopy, conductimetry and thermogravimetry. The parent ligand is a very weak carbonic anhydrase (CA) inhibitor, although it constituted the lead for developing important classes of diuretics. The complex derivatives behave as much stronger CA inhibitors, with IC50 values around 10−8 M against isozyme CA II, and 10−7 M against isozyme CAI.

scholarly journals Complexes With Biologically Active Ligands. Part 91 Metal Complexes of 5-Benzoylamino- and 5-(3-Nitrobenzoyl-Amino)-1,3,4-Thiadiazole-2-Sulfonamide as Carbonic Anhydrase Inhibitors

1997 ◽  
Vol 4 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Andrei Jitianu ◽  
Marc A. llies ◽  
Fabrizio Briganti ◽  
Andrea Scozzafava ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Metal Complexes ◽  
Elemental Analysis ◽  
Epr Spectroscopy ◽  
Biologically Active ◽  
Carbonic Anhydrase Inhibitors ◽  
Standard Procedures

Complexes containing the anions of 5-benzoylamido-1,3,4-thiadiazole-2-sulfonamide and 5-(3-nitro-benzoylamido)-1,3,4-thiadiazole-2-sulfonamid as ligands, and V(IV); Cr(III); Fe(III); Co(II); Ni(II); Cu(II) and Ag(I) were synthesized and characterized by standard procedures (elemental analysis; IR, electronic, and EPR spectroscopy; TG, magnetic and conductimetric measurements). The original sulfonamides and their metal complexes are strong inhibitors of two carbonic anhydrase (CA) isozymes, CA I and II.

Coumaronochromone as antibacterial and carbonic anhydrase inhibitors from Aerva persica (Burm.f.) Merr.: experimental and first-principles approaches

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Muhammad Imran ◽  
Ahmad Irfan ◽  
Mohammed A. Assiri ◽  
Sajjad H. Sumrra ◽  
Muhammad Saleem ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
First Principles ◽  
Molecular Electrostatic Potential ◽  
Chemical Constituents ◽  
Bacterial Strains ◽  
Hirshfeld Analysis ◽  
Carbonic Anhydrase Inhibition ◽  
Inhibition Studies ◽  
Lowest Unoccupied Molecular Orbitals

AbstractThe Aerva plants are exceptionally rich in phytochemicals and possess therapeutics potential. Phytochemical screening shows that Aerva persica (Burm.f.) Merr. contains highest contents i.e., total phenolics, flavonoids, flavonols, tannins, alkaloids, carbohydrates, anthraquinones and glycosides. In-vitro antibacterial and enzymatic (carbonic anhydrase) inhibition studies on methanol extracts of A. persica indicated the presence of biological active constituents within chloroform soluble portions. Investigation in the pure constituents on the chloroform portions of A. persica accomplished by column chromatography, NMR and MS analysis. The bioguided isolation yields four chemical constituents of coumaronochromone family, namely aervin (1-4). These pure chemical entities (1-4) showed significant antibacterial activity in the range of 60.05–79.21 µg/ml against various bacterial strains using ampicillin and ciprofloxacin as standard drugs. The compounds 1-4 showed promising carbonic anhydrase inhibition with IC50 values of 19.01, 18.24, 18.65 and 12.92 µM, respectively, using standard inhibitor acetazolamide. First-principles calculations revealed comprehensive intramolecular charge transfer in the studied compounds 1-4. The spatial distribution of highest occupied and lowest unoccupied molecular orbitals, ionization potential, molecular electrostatic potential and Hirshfeld analysis revealed that these coumaronochromone compounds would be proficient biological active compounds. These pure constituents may be used as a new pharmacophore to treat leaukomia, epilepsy, glaucoma and cystic fibrosis.

scholarly journals Carbonic Anhydrase Inhibitors Part 721 Synthesis and Antiglaucoma Properties of Metal Complexes of p-Fluorobenzolamide

1999 ◽  
Vol 6 (2) ◽  
pp. 67-73 ◽  
Author(s):  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Luca Menabuoni ◽  
Francesco Mincione ◽  
Fabrizio Briganti ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Metal Complexes ◽  
Carbonic Anhydrase Inhibitors ◽  
Physico Chemical ◽  
New Compounds

Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA) inhibitory properties, i.e., 5-(p-fluorobenzenesulfonylamido)-1,3,4-thiadiazole-2-sulfonamide (p-fluorobenzolamide) were prepared. The new complexes contained metal ions such as Zn(II), Cu(II), Co(II), Ni(II), Cd(II) and Mn(II). The new compounds were characterized by standard physico-chemical procedures, and assayed as inhibitors of three CA isozymes, CA I, II and IV. Very good inhibition has been evidenced both for the parent sulfonamides as well as for the prepared complexes, against all three investigated isozymes. Some of these new complexes as well as the parent sulfonamide, strongly lowered intraocular pressure (IOP) in normotensive rabbits when administered as a 2% solution into the eye.

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